102229-10-7Relevant articles and documents
A Convenient Procedure for the Monosilylation of Symmetric 1,n-Diols
McDougal, Patrick G.,Rico, Joseph G.,Oh, Young-Im,Condon, Brian D.
, p. 3388 - 3390 (1986)
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Novel monodisperse PEG-grafted polystyrene resins: synthesis and application in gel-phase 13C NMR spectroscopy
Braunshier, Christian,Hametner, Christian,Fr?hlich, Johannes,Schn?ller, Johannes,Hutter, Herbert
, p. 7103 - 7105 (2008)
A series of novel polystyrene-oligo(oxyethylene) graft copolymers containing monodisperse PEG units (n = 2-12) have been synthesized and examined concerning their applicability for gel-phase 13C NMR spectroscopy. A strong correlation between the graft length and the line widths in the gel-phase spectra was observed. By grafting a PEG chain with only eight units, it was possible to obtain results similar to TentaGel resin. Additionally, TOF-SIMS images were recorded in order to evaluate the homogeneity of the resin.
Selective acceleration for deprotection of benzyl ethers with ti-HMS
Itoh, Akichika,Kodama, Tomohiro,Maeda, Shiro,Masaki, Yukio
, p. 9461 - 9464 (1998)
Ti-HMS, a Ti-loaded hexagonal mesoporous silica, was found to accelerate deprotection of benzyl ethers under hydrogenolytic conditions with palladium catalyst. Such acid-sensitive functional groups as silyl ether and acetal moieties in the molecule were little affected by Ti-HMS, which possesses Lewis acid sites due to Ti-atom.
Synthesis and in vitro evaluation of e - And Z-geometrical isomers of PSS232 as potential metabotropic glutamate receptors subtype 5 (mGlu 5) binders
Sephton, Selena Milicevic,Mu, Linjing,Dragic, Martina,Kraemer, Stefanie D.,Schibli, Roger,Ametamey, Simon M.
, p. 1877 - 1885 (2013)
Based on the core structure of [11C]-ABP688, our group developed a novel fluorine-18 labeled PET radiotracer, (E)-[18F]-PSS232, with significantly improved in vivo properties compared to the earlier fluorine-18 derivative [18F]-FDEGPECO. The synthetic approach used to obtain PSS232 and the radiolabeling precursor mesylate is disclosed as well as the evaluation of the two geometrical isomers of PSS232. In vitro displacement assays showed higher binding affinity of the E-geometrical isomer (1 nM vs 15 nM, for Z-isomer), which was, for this reason, selected for radiolabeling. One-step radiolabeling conditions (K222/18F-, DMSO, 95 °C, 10 min) to synthesize (E)-[18F]-PSS232 from the mesylate via nucleophilic substitution are described. At ambient temperature, (E)-[18F]-PSS232, with log D7.4 value of 2.0, was chemically stable over six hours in the presence of sodium ascorbate as a radical scavenger. Georg Thieme Verlag Stuttgart · New York.
PRODRUGS OF THE TYROSINE KINASE INHIBITOR FOR TREATING CANCER
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Paragraph 00192-00193, (2021/03/05)
There are provided compounds of Formula (I), and pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions thereof, useful for inhibition or modulation of the activity of tyrosine kinases and treatment of disease states or conditions mediated by tyrosine kinases, including cancers. (I)
Stereoselective synthesis of new pyran-dioxane based polycycles from glycal derived vinyl epoxide
Barbini, Gabriele,Di Bussolo, Valeria,Di Pietro, Sebastiano,Favero, Lucilla,Iacopini, Dalila,Pineschi, Mauro
, p. 9190 - 9198 (2021/11/16)
Chiral heteropolycyclic structures are widespread in compounds of high pharmaceutical relevance. In particular, linear fused pyran-dioxane based polycycles can be found in several naturally occurring molecules, and among them, cardiac glycosides and antibiotic spectinomycin are characterized by a cis-cisoid-trans geometry. Then, the stereocontrol in the synthesis of this type of polycyclic scaffold is of primary importance. Herein, we present two novel linear fused pyran-dioxane based bi- and tricycles, synthesized with total stereoselectivity from a glycal derived vinyl epoxide. The straightforward methodology described involves a substrate-dependent stereospecific glycosylation step followed by an intramolecular SN2′ conjugate addition process, leading to a pyran-dioxane-cyclohexane tricycle with a cis-cisoid-trans stereochemistry, in agreement with the geometry of many natural products. The stereochemical analysis of these compounds, which was realized by a combined NMR/computational approach, is also reported. This journal is
A pharmaceutical intermediate of PROTAC molecules targeting monoacylglycerol lipase. Preparation method and application
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Paragraph 0097; 0103-0104, (2021/10/27)
The invention discloses a medical intermediate of PROTAC molecules targeting monoacylglycerol lipase, a preparation method and an application thereof, and relates to the field of medicines. It has the structure shown I: formula I. The hydroxyl end has the
